product name Lopinavir
Description: Lopinavir (also known as ABT-378) is a highly potent HIV protease inhibitor with Ki of 1.3 pM in a cell-free assay. Lopinavir, a ritonavir analog designed to have a diminished interaction with Val82 in HIV protease, maintains a high potency inhibiting Val82 mutant HIV selected by ritonavir with 50% effective concentration EC50 value lower than 0.06 μM. Although the antiviral activity of ritonavir is considerably attenuated by human serum, lopinavir is less affected by human serum proteins and is 10-fold greater in potency than ritonavir in the presence of human serum.
References: Antimicrob Agents Chemother. 1998 Dec;42(12):3218-24; Drug Metab Dispos. 1999 Jan;27(1):86-91.
628.8
Formula
C37H48N4O5
CAS No.
192725-17-0
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 126 mg/mL (200.4 mM)
Water: <1 mg/mL
Ethanol: 126 mg/mL (200.4 mM)
Solubility (In vivo)
30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL
Synonyms
ABT-378
other peoduct :
| In Vitro |
In vitro activity: Lopinavir binds to mutant HIV protease (V82A, V82F and V82T) with Ki of 4.9 pM, 3.7 pM and 3.6 pM, respectively. Lopinavir inhibits 93% of wild-type HIV protease activity at 0.5 nM. Lopinavir inhibits HIV protease activity in the absence and presence of 50% HS with EC50 of 17 nM and 102 nM, respectively, in MT4 cells. Lopinavir is converted to several metabolites in an NADPH-dependent manner in liver microsomes with the primary metabolites M-3 and M-4. Lopinavir is a potent inhibitor of Rh123 efflux in Caco-2 monolayers with IC50 of 1.7 mM. Lopinavir exposure (72 hours) in LS 180V cells reduces the content of intracellular Rh123. Lopinavir induces P-glycoprotein immunoreactive protein and messenger RNA levels in LS 180V cells. Lopinavir inhibits subtype C clone C6 with IC50 of 9.4 nM. Lopinavir inhibits CYP3A with IC50 of 7.3 mM in human liver microsomes, while produces negligible or weak inhibition of human CYP1A2, 2B6, 2C9, 2C19 and 2D6. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Lopinavir (10 mg/kg, orally) results in Cmax of 0.8 μg/mL and oral bioavailability of 25% in rats. |
| Animal model | Sprague-Dawley-derived rats or cynomolgus monkeys |
| Formulation & Dosage | Dissolved in ethanol-propylene glycol-D5W;10 mg/kg; p.o. |
| References | Antimicrob Agents Chemother. 1998 Dec;42(12):3218-24; Drug Metab Dispos. 1999 Jan;27(1):86-91. |
